HUP0401984A2 - A 4. tipusú foszfodiészteráz enzim aktivitását gátló inhibitorok alkalmazása gyógyszerkészítmények előállítására és más hatóanyagokkal alkotott kombinációik - Google Patents

A 4. tipusú foszfodiészteráz enzim aktivitását gátló inhibitorok alkalmazása gyógyszerkészítmények előállítására és más hatóanyagokkal alkotott kombinációik

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Publication number
HUP0401984A2
HUP0401984A2 HU0401984A HUP0401984A HUP0401984A2 HU P0401984 A2 HUP0401984 A2 HU P0401984A2 HU 0401984 A HU0401984 A HU 0401984A HU P0401984 A HUP0401984 A HU P0401984A HU P0401984 A2 HUP0401984 A2 HU P0401984A2
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Hungary
Prior art keywords
atom
group
inhibitors
atoms
mean
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HU0401984A
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English (en)
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Hans-Michael Eggenweiler
Michael Wolf
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Merck Patent Gmbh
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Publication of HUP0401984A2 publication Critical patent/HUP0401984A2/hu
Publication of HUP0401984A3 publication Critical patent/HUP0401984A3/hu

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
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Abstract

A találmány a 4. típusú foszfodiészteráz enzim aktivitását gátlóinhibitorok (PDE IV inhibitorok) gyógyszerek előállítását célzóalkalmazására és a PDE IV inhibitorok más hatóanyagokkal alkotottkombinációira vonatkozik. A találmány többek között az (I) általánosképletű vegyületeknek és azok sztereoizomereinek, továbbá fiziológiaiszempontból elfogadható sóinak és szolvátjainak olyan gyógyszerekelőállítását célzó alkalmazására vonatkozik, amelyekkel kezelni lehetaz olyan betegeket, akiknek a betegsége vagy kóros állapotaösszefüggésben van a PDE4-izoenzimnek azzal a szerepével, amelyet azeozinnal megfesthető emberi sejtek (humán eozinofilek) aktiválódásánakés degranulálódásának a szabályozásában játszik. Az (I) általánosképletben B jelentése nitrogénatomon vagy szénatomon keresztülkapcsolódó, 1-4 nitrogén-, oxigén- és/vagy kénatomot tartalmazó,helyettesítetlen vagy halogénatommal, A-val és/vagy OA-val mono-, di-vagy triszubsztituált aromás heterociklusos csoport, amelybenzolgyűrűvel vagy piridingyűrűvel kondenzált is lehet; Q nincs jelenvagy 1-6 szénatomos alkiléncsoportot jelent; X jelentése CH2, S vagyO; R1 és R2 jelentése - egymástól függetlenül - hidrogénatom vagy A;R3 és R4 jelentése - egymástól függetlenül - -OH, OR5, -S-R5, -SO-R5,-SO2-R5, Hal, metilén-dioxi-csoport, -NO2, -NH2, -NHR5 vagy -NR5R6; R5és R6 jelentése - egymástól függetlenül - A, 3-7 szénatomoscikloalkilcsoport, 4-8 szénatomos metilén-cikloalkil-csoport vagy 2-8szénatomos alkenilcsoport; A jelentése 1-10 szénatomos alkilcsoport,amely 1-5 fluoratommal és/vagy klóratommal helyettesítve lehet; és Haljelentése fluoratom, klóratom, brómatom vagy jódatom; Ó
HU0401984A 2001-10-31 2002-08-28 Use of type 4 phosphodiesterase inhibitors for preparation of pharmaceutical compositions and combination with other active ingredients HUP0401984A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01125394 2001-10-31
PCT/EP2002/009596 WO2003037349A1 (en) 2001-10-31 2002-08-28 Type 4 phosphodiesterase inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
HUP0401984A2 true HUP0401984A2 (hu) 2005-02-28
HUP0401984A3 HUP0401984A3 (en) 2005-06-28

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HU0401984A HUP0401984A3 (en) 2001-10-31 2002-08-28 Use of type 4 phosphodiesterase inhibitors for preparation of pharmaceutical compositions and combination with other active ingredients

Country Status (12)

Country Link
US (1) US20040259863A1 (hu)
EP (1) EP1463509A1 (hu)
JP (1) JP2005515975A (hu)
CN (1) CN1578665A (hu)
AR (1) AR037743A1 (hu)
CA (1) CA2462525A1 (hu)
CZ (1) CZ2004516A3 (hu)
HU (1) HUP0401984A3 (hu)
MX (1) MXPA04003668A (hu)
NO (1) NO20042229L (hu)
SK (1) SK1862004A3 (hu)
WO (1) WO2003037349A1 (hu)

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US20040259863A1 (en) 2004-12-23
WO2003037349A1 (en) 2003-05-08
MXPA04003668A (es) 2004-07-22
CZ2004516A3 (cs) 2004-08-18
SK1862004A3 (en) 2004-08-03
JP2005515975A (ja) 2005-06-02
HUP0401984A3 (en) 2005-06-28
CA2462525A1 (en) 2003-05-08
AR037743A1 (es) 2004-12-01
NO20042229L (no) 2004-05-28
EP1463509A1 (en) 2004-10-06

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